US6159449A - Dentifrice products and methods for remineralizing and/or mineralizing teeth - Google Patents
Dentifrice products and methods for remineralizing and/or mineralizing teeth Download PDFInfo
- Publication number
- US6159449A US6159449A US08/832,827 US83282797A US6159449A US 6159449 A US6159449 A US 6159449A US 83282797 A US83282797 A US 83282797A US 6159449 A US6159449 A US 6159449A
- Authority
- US
- United States
- Prior art keywords
- water
- soluble
- cationic
- magnesium
- fluoride
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 230000000395 remineralizing effect Effects 0.000 title claims abstract description 30
- 230000001089 mineralizing effect Effects 0.000 title claims abstract description 23
- 238000000034 method Methods 0.000 title claims description 36
- 239000000551 dentifrice Substances 0.000 title abstract description 53
- 125000002091 cationic group Chemical group 0.000 claims abstract description 135
- 125000000129 anionic group Chemical group 0.000 claims abstract description 122
- 239000000203 mixture Substances 0.000 claims abstract description 117
- -1 fluoride compound Chemical class 0.000 claims abstract description 113
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 61
- 210000003296 saliva Anatomy 0.000 claims abstract description 53
- 150000002681 magnesium compounds Chemical class 0.000 claims abstract description 39
- 230000003902 lesion Effects 0.000 claims abstract description 36
- 229940043430 calcium compound Drugs 0.000 claims abstract description 32
- 150000001674 calcium compounds Chemical class 0.000 claims abstract description 28
- 210000005239 tubule Anatomy 0.000 claims abstract description 27
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical class [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims abstract description 25
- 238000002156 mixing Methods 0.000 claims abstract description 18
- 239000000047 product Substances 0.000 claims description 166
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims description 81
- 239000011575 calcium Substances 0.000 claims description 56
- 229910052791 calcium Inorganic materials 0.000 claims description 56
- 229960005069 calcium Drugs 0.000 claims description 52
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 40
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical group [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 34
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims description 32
- 239000011777 magnesium Substances 0.000 claims description 30
- 229910052749 magnesium Inorganic materials 0.000 claims description 30
- 229940091250 magnesium supplement Drugs 0.000 claims description 30
- 239000000499 gel Substances 0.000 claims description 29
- JLVVSXFLKOJNIY-UHFFFAOYSA-N Magnesium ion Chemical compound [Mg+2] JLVVSXFLKOJNIY-UHFFFAOYSA-N 0.000 claims description 27
- 239000007864 aqueous solution Substances 0.000 claims description 27
- 229910001425 magnesium ion Inorganic materials 0.000 claims description 26
- 159000000007 calcium salts Chemical class 0.000 claims description 25
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 24
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 22
- 239000000606 toothpaste Substances 0.000 claims description 18
- 239000011775 sodium fluoride Substances 0.000 claims description 17
- 235000013024 sodium fluoride Nutrition 0.000 claims description 17
- 229960002337 magnesium chloride Drugs 0.000 claims description 16
- 229910001629 magnesium chloride Inorganic materials 0.000 claims description 16
- 235000011147 magnesium chloride Nutrition 0.000 claims description 16
- 239000002609 medium Substances 0.000 claims description 15
- 239000006072 paste Substances 0.000 claims description 14
- 239000000463 material Substances 0.000 claims description 13
- 150000001450 anions Chemical class 0.000 claims description 11
- 239000002324 mouth wash Substances 0.000 claims description 11
- MKJXYGKVIBWPFZ-UHFFFAOYSA-L calcium lactate Chemical compound [Ca+2].CC(O)C([O-])=O.CC(O)C([O-])=O MKJXYGKVIBWPFZ-UHFFFAOYSA-L 0.000 claims description 10
- 239000001527 calcium lactate Substances 0.000 claims description 10
- 235000011086 calcium lactate Nutrition 0.000 claims description 10
- 229940095672 calcium sulfate Drugs 0.000 claims description 10
- 235000015218 chewing gum Nutrition 0.000 claims description 10
- 150000001768 cations Chemical class 0.000 claims description 8
- 150000004673 fluoride salts Chemical class 0.000 claims description 7
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims description 6
- ZCCIPPOKBCJFDN-UHFFFAOYSA-N calcium nitrate Chemical compound [Ca+2].[O-][N+]([O-])=O.[O-][N+]([O-])=O ZCCIPPOKBCJFDN-UHFFFAOYSA-N 0.000 claims description 6
- 159000000003 magnesium salts Chemical class 0.000 claims description 6
- 239000012736 aqueous medium Substances 0.000 claims description 5
- VSGNNIFQASZAOI-UHFFFAOYSA-L calcium acetate Chemical compound [Ca+2].CC([O-])=O.CC([O-])=O VSGNNIFQASZAOI-UHFFFAOYSA-L 0.000 claims description 5
- 239000001639 calcium acetate Substances 0.000 claims description 5
- 235000011092 calcium acetate Nutrition 0.000 claims description 5
- 229960005147 calcium acetate Drugs 0.000 claims description 5
- 229920002678 cellulose Polymers 0.000 claims description 5
- 239000001913 cellulose Substances 0.000 claims description 5
- 239000002244 precipitate Substances 0.000 claims description 5
- 239000003826 tablet Substances 0.000 claims description 5
- UEGPKNKPLBYCNK-UHFFFAOYSA-L magnesium acetate Chemical compound [Mg+2].CC([O-])=O.CC([O-])=O UEGPKNKPLBYCNK-UHFFFAOYSA-L 0.000 claims description 4
- 239000011654 magnesium acetate Substances 0.000 claims description 4
- 235000011285 magnesium acetate Nutrition 0.000 claims description 4
- 229940069446 magnesium acetate Drugs 0.000 claims description 4
- YIXJRHPUWRPCBB-UHFFFAOYSA-N magnesium nitrate Chemical compound [Mg+2].[O-][N+]([O-])=O.[O-][N+]([O-])=O YIXJRHPUWRPCBB-UHFFFAOYSA-N 0.000 claims description 4
- 229920001577 copolymer Polymers 0.000 claims description 3
- 235000013305 food Nutrition 0.000 claims description 3
- 239000007937 lozenge Substances 0.000 claims description 3
- 229910052943 magnesium sulfate Inorganic materials 0.000 claims description 3
- 229960003390 magnesium sulfate Drugs 0.000 claims description 3
- 235000019341 magnesium sulphate Nutrition 0.000 claims description 3
- 230000000069 prophylactic effect Effects 0.000 claims description 3
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 claims description 3
- 229960002799 stannous fluoride Drugs 0.000 claims description 3
- 229920002554 vinyl polymer Polymers 0.000 claims description 3
- JKNCOURZONDCGV-UHFFFAOYSA-N 2-(dimethylamino)ethyl 2-methylprop-2-enoate Chemical compound CN(C)CCOC(=O)C(C)=C JKNCOURZONDCGV-UHFFFAOYSA-N 0.000 claims description 2
- KGIGUEBEKRSTEW-UHFFFAOYSA-N 2-vinylpyridine Chemical compound C=CC1=CC=CC=N1 KGIGUEBEKRSTEW-UHFFFAOYSA-N 0.000 claims description 2
- DDFHBQSCUXNBSA-UHFFFAOYSA-N 5-(5-carboxythiophen-2-yl)thiophene-2-carboxylic acid Chemical compound S1C(C(=O)O)=CC=C1C1=CC=C(C(O)=O)S1 DDFHBQSCUXNBSA-UHFFFAOYSA-N 0.000 claims description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 2
- 239000001856 Ethyl cellulose Substances 0.000 claims description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 2
- 229920001800 Shellac Polymers 0.000 claims description 2
- UGLUPDDGTQHFKU-UHFFFAOYSA-M [NH4+].S(=O)(=O)([O-])[O-].[Mg+] Chemical compound [NH4+].S(=O)(=O)([O-])[O-].[Mg+] UGLUPDDGTQHFKU-UHFFFAOYSA-M 0.000 claims description 2
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims description 2
- 229940095564 anhydrous calcium sulfate Drugs 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 239000001110 calcium chloride Substances 0.000 claims description 2
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 2
- 229960002713 calcium chloride Drugs 0.000 claims description 2
- 239000004227 calcium gluconate Substances 0.000 claims description 2
- 235000013927 calcium gluconate Nutrition 0.000 claims description 2
- 229960004494 calcium gluconate Drugs 0.000 claims description 2
- OLOZVPHKXALCRI-UHFFFAOYSA-L calcium malate Chemical compound [Ca+2].[O-]C(=O)C(O)CC([O-])=O OLOZVPHKXALCRI-UHFFFAOYSA-L 0.000 claims description 2
- 239000001362 calcium malate Substances 0.000 claims description 2
- 229940016114 calcium malate Drugs 0.000 claims description 2
- 235000011038 calcium malates Nutrition 0.000 claims description 2
- ZOMBKNNSYQHRCA-UHFFFAOYSA-J calcium sulfate hemihydrate Chemical compound O.[Ca+2].[Ca+2].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O ZOMBKNNSYQHRCA-UHFFFAOYSA-J 0.000 claims description 2
- GUPPESBEIQALOS-UHFFFAOYSA-L calcium tartrate Chemical compound [Ca+2].[O-]C(=O)C(O)C(O)C([O-])=O GUPPESBEIQALOS-UHFFFAOYSA-L 0.000 claims description 2
- 235000011035 calcium tartrate Nutrition 0.000 claims description 2
- 239000001427 calcium tartrate Substances 0.000 claims description 2
- NEEHYRZPVYRGPP-UHFFFAOYSA-L calcium;2,3,4,5,6-pentahydroxyhexanoate Chemical compound [Ca+2].OCC(O)C(O)C(O)C(O)C([O-])=O.OCC(O)C(O)C(O)C(O)C([O-])=O NEEHYRZPVYRGPP-UHFFFAOYSA-L 0.000 claims description 2
- PBUBJNYXWIDFMU-UHFFFAOYSA-L calcium;butanedioate Chemical compound [Ca+2].[O-]C(=O)CCC([O-])=O PBUBJNYXWIDFMU-UHFFFAOYSA-L 0.000 claims description 2
- MLMODXBPCNLAGP-UHFFFAOYSA-L calcium;propanedioate Chemical compound [Ca+2].[O-]C(=O)CC([O-])=O MLMODXBPCNLAGP-UHFFFAOYSA-L 0.000 claims description 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 2
- 229920001249 ethyl cellulose Polymers 0.000 claims description 2
- 239000003925 fat Substances 0.000 claims description 2
- PJJZFXPJNUVBMR-UHFFFAOYSA-L magnesium benzoate Chemical compound [Mg+2].[O-]C(=O)C1=CC=CC=C1.[O-]C(=O)C1=CC=CC=C1 PJJZFXPJNUVBMR-UHFFFAOYSA-L 0.000 claims description 2
- OTCKOJUMXQWKQG-UHFFFAOYSA-L magnesium bromide Chemical compound [Mg+2].[Br-].[Br-] OTCKOJUMXQWKQG-UHFFFAOYSA-L 0.000 claims description 2
- 229910001623 magnesium bromide Inorganic materials 0.000 claims description 2
- 239000004337 magnesium citrate Substances 0.000 claims description 2
- 229960005336 magnesium citrate Drugs 0.000 claims description 2
- 235000002538 magnesium citrate Nutrition 0.000 claims description 2
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims description 2
- CQQJGTPWCKCEOQ-UHFFFAOYSA-L magnesium dipropionate Chemical compound [Mg+2].CCC([O-])=O.CCC([O-])=O CQQJGTPWCKCEOQ-UHFFFAOYSA-L 0.000 claims description 2
- 239000001755 magnesium gluconate Substances 0.000 claims description 2
- 235000015778 magnesium gluconate Nutrition 0.000 claims description 2
- 229960003035 magnesium gluconate Drugs 0.000 claims description 2
- 239000000347 magnesium hydroxide Substances 0.000 claims description 2
- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims description 2
- 229960000816 magnesium hydroxide Drugs 0.000 claims description 2
- 235000012254 magnesium hydroxide Nutrition 0.000 claims description 2
- BLQJIBCZHWBKSL-UHFFFAOYSA-L magnesium iodide Chemical compound [Mg+2].[I-].[I-] BLQJIBCZHWBKSL-UHFFFAOYSA-L 0.000 claims description 2
- 229910001641 magnesium iodide Inorganic materials 0.000 claims description 2
- OVGXLJDWSLQDRT-UHFFFAOYSA-L magnesium lactate Chemical compound [Mg+2].CC(O)C([O-])=O.CC(O)C([O-])=O OVGXLJDWSLQDRT-UHFFFAOYSA-L 0.000 claims description 2
- 229940095060 magnesium tartrate Drugs 0.000 claims description 2
- OVGXLJDWSLQDRT-JCWNAWFTSA-L magnesium;(2r)-2-hydroxypropanoate Chemical compound [Mg+2].C[C@@H](O)C([O-])=O.C[C@@H](O)C([O-])=O OVGXLJDWSLQDRT-JCWNAWFTSA-L 0.000 claims description 2
- MUZDLCBWNVUYIR-ZVGUSBNCSA-L magnesium;(2r,3r)-2,3-dihydroxybutanedioate Chemical compound [Mg+2].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O MUZDLCBWNVUYIR-ZVGUSBNCSA-L 0.000 claims description 2
- IAKLPCRFBAZVRW-XRDLMGPZSA-L magnesium;(2r,3s,4r,5r)-2,3,4,5,6-pentahydroxyhexanoate;hydrate Chemical compound O.[Mg+2].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O IAKLPCRFBAZVRW-XRDLMGPZSA-L 0.000 claims description 2
- 229940044652 phenolsulfonate Drugs 0.000 claims description 2
- 239000004208 shellac Substances 0.000 claims description 2
- 229940113147 shellac Drugs 0.000 claims description 2
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 claims description 2
- 235000013874 shellac Nutrition 0.000 claims description 2
- PLSARIKBYIPYPF-UHFFFAOYSA-H trimagnesium dicitrate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O PLSARIKBYIPYPF-UHFFFAOYSA-H 0.000 claims description 2
- NFMWFGXCDDYTEG-UHFFFAOYSA-N trimagnesium;diborate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]B([O-])[O-].[O-]B([O-])[O-] NFMWFGXCDDYTEG-UHFFFAOYSA-N 0.000 claims description 2
- 239000001993 wax Substances 0.000 claims description 2
- 239000004698 Polyethylene Substances 0.000 claims 1
- 229910001515 alkali metal fluoride Inorganic materials 0.000 claims 1
- 229940041131 calcium lactate gluconate Drugs 0.000 claims 1
- 229920001971 elastomer Polymers 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229920000573 polyethylene Polymers 0.000 claims 1
- 229920002689 polyvinyl acetate Polymers 0.000 claims 1
- 239000011118 polyvinyl acetate Substances 0.000 claims 1
- 229920000915 polyvinyl chloride Polymers 0.000 claims 1
- 239000004800 polyvinyl chloride Substances 0.000 claims 1
- 239000005060 rubber Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 abstract description 19
- 238000005498 polishing Methods 0.000 abstract description 12
- 229910019142 PO4 Inorganic materials 0.000 abstract description 6
- 239000010452 phosphate Substances 0.000 abstract description 6
- 229940091249 fluoride supplement Drugs 0.000 description 110
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 50
- LRCFXGAMWKDGLA-UHFFFAOYSA-N dioxosilane;hydrate Chemical compound O.O=[Si]=O LRCFXGAMWKDGLA-UHFFFAOYSA-N 0.000 description 41
- 229960004029 silicic acid Drugs 0.000 description 41
- 239000000243 solution Substances 0.000 description 34
- 150000003839 salts Chemical class 0.000 description 31
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 30
- 210000000214 mouth Anatomy 0.000 description 27
- 239000002562 thickening agent Substances 0.000 description 26
- 239000000796 flavoring agent Substances 0.000 description 25
- 235000011187 glycerol Nutrition 0.000 description 25
- 239000001506 calcium phosphate Substances 0.000 description 23
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 22
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 22
- 229910001424 calcium ion Inorganic materials 0.000 description 22
- 235000019634 flavors Nutrition 0.000 description 22
- 229910052751 metal Inorganic materials 0.000 description 22
- 239000002184 metal Substances 0.000 description 22
- 239000000600 sorbitol Substances 0.000 description 22
- 230000033558 biomineral tissue development Effects 0.000 description 21
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 21
- 229940050906 magnesium chloride hexahydrate Drugs 0.000 description 20
- DHRRIBDTHFBPNG-UHFFFAOYSA-L magnesium dichloride hexahydrate Chemical compound O.O.O.O.O.O.[Mg+2].[Cl-].[Cl-] DHRRIBDTHFBPNG-UHFFFAOYSA-L 0.000 description 20
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 20
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 20
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 20
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 20
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 19
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 19
- 210000003298 dental enamel Anatomy 0.000 description 19
- 229910052588 hydroxylapatite Inorganic materials 0.000 description 19
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 18
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 18
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 16
- 208000002925 dental caries Diseases 0.000 description 16
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 16
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 description 15
- 229910001634 calcium fluoride Inorganic materials 0.000 description 15
- 150000002500 ions Chemical class 0.000 description 15
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 14
- 235000011010 calcium phosphates Nutrition 0.000 description 14
- 150000002222 fluorine compounds Chemical class 0.000 description 14
- 229910052708 sodium Inorganic materials 0.000 description 14
- 239000011734 sodium Substances 0.000 description 14
- 229940034610 toothpaste Drugs 0.000 description 14
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 13
- 239000002253 acid Substances 0.000 description 13
- 238000009472 formulation Methods 0.000 description 13
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 12
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 12
- 230000015572 biosynthetic process Effects 0.000 description 12
- 229910000389 calcium phosphate Inorganic materials 0.000 description 12
- 238000006243 chemical reaction Methods 0.000 description 12
- 239000004615 ingredient Substances 0.000 description 12
- 229920001213 Polysorbate 20 Polymers 0.000 description 10
- RBLGLDWTCZMLRW-UHFFFAOYSA-K dicalcium;phosphate;dihydrate Chemical compound O.O.[Ca+2].[Ca+2].[O-]P([O-])([O-])=O RBLGLDWTCZMLRW-UHFFFAOYSA-K 0.000 description 10
- 230000000694 effects Effects 0.000 description 10
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 10
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 10
- 229960002216 methylparaben Drugs 0.000 description 10
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 10
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 10
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 10
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 10
- 229960003415 propylparaben Drugs 0.000 description 10
- 229910052712 strontium Inorganic materials 0.000 description 10
- CIOAGBVUUVVLOB-UHFFFAOYSA-N strontium atom Chemical compound [Sr] CIOAGBVUUVVLOB-UHFFFAOYSA-N 0.000 description 10
- 229910001631 strontium chloride Inorganic materials 0.000 description 10
- AHBGXTDRMVNFER-UHFFFAOYSA-L strontium dichloride Chemical compound [Cl-].[Cl-].[Sr+2] AHBGXTDRMVNFER-UHFFFAOYSA-L 0.000 description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 9
- 229960002401 calcium lactate Drugs 0.000 description 9
- 230000008569 process Effects 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 8
- 239000004310 lactic acid Substances 0.000 description 8
- 235000014655 lactic acid Nutrition 0.000 description 8
- 229920001223 polyethylene glycol Polymers 0.000 description 8
- 240000002834 Paulownia tomentosa Species 0.000 description 7
- 235000010678 Paulownia tomentosa Nutrition 0.000 description 7
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 7
- 239000003082 abrasive agent Substances 0.000 description 7
- 229910000019 calcium carbonate Inorganic materials 0.000 description 7
- 229960003563 calcium carbonate Drugs 0.000 description 7
- 235000010216 calcium carbonate Nutrition 0.000 description 7
- 229940112822 chewing gum Drugs 0.000 description 7
- 239000003906 humectant Substances 0.000 description 7
- ZDGGJQMSELMHLK-UHFFFAOYSA-N m-Trifluoromethylhippuric acid Chemical compound OC(=O)CNC(=O)C1=CC=CC(C(F)(F)F)=C1 ZDGGJQMSELMHLK-UHFFFAOYSA-N 0.000 description 7
- 229940074371 monofluorophosphate Drugs 0.000 description 7
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 7
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- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 235000010494 karaya gum Nutrition 0.000 description 1
- 239000011133 lead Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 239000007791 liquid phase Substances 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 229960001708 magnesium carbonate Drugs 0.000 description 1
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- WPBNNNQJVZRUHP-UHFFFAOYSA-L manganese(2+);methyl n-[[2-(methoxycarbonylcarbamothioylamino)phenyl]carbamothioyl]carbamate;n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[S-]C(=S)NCCNC([S-])=S.COC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OC WPBNNNQJVZRUHP-UHFFFAOYSA-L 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 150000002736 metal compounds Chemical class 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
- 125000005341 metaphosphate group Chemical group 0.000 description 1
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- 229940005638 monofluorophosphate ion Drugs 0.000 description 1
- 235000019960 monoglycerides of fatty acid Nutrition 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 1
- 235000019796 monopotassium phosphate Nutrition 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- 235000019659 mouth feeling Nutrition 0.000 description 1
- 229920001206 natural gum Polymers 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 229910052759 nickel Inorganic materials 0.000 description 1
- DBJLJFTWODWSOF-UHFFFAOYSA-L nickel(ii) fluoride Chemical compound F[Ni]F DBJLJFTWODWSOF-UHFFFAOYSA-L 0.000 description 1
- 150000002823 nitrates Chemical class 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- BHZSLLSDZFAPFH-UHFFFAOYSA-L palladium(2+);difluoride Chemical compound F[Pd]F BHZSLLSDZFAPFH-UHFFFAOYSA-L 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- 229940085991 phosphate ion Drugs 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical class [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 1
- 238000010944 pre-mature reactiony Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000008439 repair process Effects 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 238000007788 roughening Methods 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 229910002028 silica xerogel Inorganic materials 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 229960001462 sodium cyclamate Drugs 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical class [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 229940080264 sodium dodecylbenzenesulfonate Drugs 0.000 description 1
- BFDWBSRJQZPEEB-UHFFFAOYSA-L sodium fluorophosphate Chemical compound [Na+].[Na+].[O-]P([O-])(F)=O BFDWBSRJQZPEEB-UHFFFAOYSA-L 0.000 description 1
- 235000019983 sodium metaphosphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
- 235000019408 sucralose Nutrition 0.000 description 1
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 239000000271 synthetic detergent Substances 0.000 description 1
- 229940104261 taurate Drugs 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229920001187 thermosetting polymer Polymers 0.000 description 1
- 239000011135 tin Substances 0.000 description 1
- YUOWTJMRMWQJDA-UHFFFAOYSA-J tin(iv) fluoride Chemical compound [F-].[F-].[F-].[F-].[Sn+4] YUOWTJMRMWQJDA-UHFFFAOYSA-J 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 239000011573 trace mineral Substances 0.000 description 1
- 235000013619 trace mineral Nutrition 0.000 description 1
- 229910000404 tripotassium phosphate Inorganic materials 0.000 description 1
- 235000019798 tripotassium phosphate Nutrition 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical class [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 229910000406 trisodium phosphate Chemical class 0.000 description 1
- 235000019801 trisodium phosphate Nutrition 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 239000009637 wintergreen oil Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000010457 zeolite Substances 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
- OMQSJNWFFJOIMO-UHFFFAOYSA-J zirconium tetrafluoride Chemical compound F[Zr](F)(F)F OMQSJNWFFJOIMO-UHFFFAOYSA-J 0.000 description 1
- GFQYVLUOOAAOGM-UHFFFAOYSA-N zirconium(iv) silicate Chemical compound [Zr+4].[O-][Si]([O-])([O-])[O-] GFQYVLUOOAAOGM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/20—Halogens; Compounds thereof
- A61K8/21—Fluorides; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/88—Two- or multipart kits
Definitions
- This invention relates to dentifrice products and methods for remineralizing and/or mineralizing teeth. More particularly, this invention relates to fluoride-containing dentifrice products and methods of using same to achieve improved remineralization of subsurface carious lesions and/or mineralization of exposed dentinal tubules.
- Dental caries i.e., tooth decay, is a leading cause of tooth damage in humans.
- Dental caries begins with lesions of so-called "white spots", which are demineralized areas below the surface of intact dental enamel. Such subsurface lesions are formed before a cavity is detectable. If unchecked, surface enamel above a subsurface lesion eventually collapses, leading to cavitation and subsequent loss of tooth structure.
- Dental caries is typically caused by the presence of acids in the oral cavity. This is because the primary component of the enamel and dentin in teeth is calcium hydroxyapatite, which, though highly insoluble at normal oral pHs, is relatively soluble in acid media. Thus, when a tooth is exposed to acids, e.g., acids formed during the glycolysis of sugar caused by various oral bacteria, carious lesions can form in the enamel and dentin of the tooth.
- acids e.g., acids formed during the glycolysis of sugar caused by various oral bacteria
- compositions and methods for preventing or reducing dental caries are known in the art.
- compositions and methods which use remineralization to retard or arrest dental caries are known in the art.
- U.S. Pat. No. 4,080,440 discloses a method for remineralizing tooth enamel involving forming a metastable mixture having a low pH (between 2.5 and 4.0) by mixing a solution containing a soluble calcium salt and preferably a soluble salt of a heavy metal or magnesium with a solution containing a soluble phosphate salt and preferably a soluble fluoride salt, and then applying the metastable mixture to the tooth surface.
- a significant disadvantage of the use of metastable solutions is that the relatively low pH might demineralize the dental enamel and/or injure other tissue.
- U.S. Pat. Nos. 4,177,258, 4,183,915 and 4,348,381 disclose a remineralizing solution containing supersaturated concentrations of calcium ions, phosphate ions and a fluoride source stabilized by the present of an antinucleating agent such as diamine tetramethylenephosphonic acid, ethylenediamine tetramethylenephosphonic acid and 2-phosphonobutane-tricarboxylic acid-1,2,4, or the water-soluble salts thereof.
- This solution is preferably adjusted to the neutral pH range where the solution is alleged to most effectively remineralize subsurface lesions. Even though the antinucleating agent would be expected to stabilize the solution, equilibrium of the supersaturated concentrations is still found difficult to maintain and avoid precipitation of hydroxyapatite and changes in the pH of the solution.
- U.S. Pat. Nos. 4,083,955 (Grabenstetter et al) and 4,397,837 (Raaf et al) disclose a process for remineralizing demineralized enamel by the consecutive treatment of tooth surfaces with separate solutions containing calcium ions and phosphate ions.
- the solution containing the calcium ions may further contain heavy metal ions or magnesium ions, while the solution containing the phosphate ions may also contain fluoride ions.
- By sequentially applying calcium and phosphate ions to the tooth surface high concentrations of the ions are able to penetrate into lesions in solution form, where the ions precipitate as a calcium phosphate salt when ions from the second treatment solution diffuse in. While apparently successful, this method involves the inconvenience of a plurality of sequential applications, which can also be time consuming.
- U.S. Pat. Nos. 4,606,912 and 4,610,873 teach methods of making clear aqueous mouthwash solutions which totally prevent formation of calcium phosphate crystals, e.g., hydroxyapatite.
- the solutions are capable of remineralizing lesions in teeth and are prepared by initially forming a solution containing a source of calcium ions and a chelating agent for calcium ions, causing the chelation of at least 50% of the calcium ions and subsequently adding a source of phosphate ions to the aqueous solution.
- a source of calcium ions e.g., hydroxyapatite
- a chelating agent for calcium ions e.g., a chelating agent for calcium ions
- U.S. Pat. No. 3,679,360 to Rubin et al. discloses a remineralization method the purpose of which is to deposit calcium phosphate from a gel medium onto the surface of a tooth.
- This method of remineralization has several disadvantages. For example, in the Rubin et al. method, remineralization occurs only on the surface of a tooth whereas the initial cause of dental caries is subsurface demineralization. Furthermore, in the Rubin et al. method, the surface on which apatite growth is desired must be prepared (as by roughening), and the tooth and coatings must be covered by a suitable cap for several days while the mineralization of the tooth surface occurs.
- U.S. Pat. Nos. 5,037,639; 5,268,167; 5,437,857; 5,427,768; and 5,460,803 teach the use of amorphous calcium compounds such as amorphous calcium phosphate (ACP), amorphous calcium phosphate fluoride (ACPF) and amorphous calcium carbonate phosphate (ACCP) for use in remineralizing teeth.
- ACP amorphous calcium phosphate
- ACPF amorphous calcium phosphate fluoride
- ACCP amorphous calcium carbonate phosphate
- These amorphous compounds or solutions which form the amorphous compounds when applied either onto or into dental tissue prevent and/or repair dental weaknesses such as dental caries, exposed roots and dentin sensitivity.
- the compounds are claimed to have high solubilities, fast formation rates and fast conversion rates (to apatite).
- remineralization is accomplished by bringing the amorphous compound into contact with the dental tissue. This can be done directly, i.e., putting an amorphous compound directly on the tooth, or indirectly through a carrier, i.e., incorporating the amorphous compound in a carrier such as a gel, a chewing gum, or a toothpaste and applying the carrier to the dental tissue.
- a carrier i.e., incorporating the amorphous compound in a carrier such as a gel, a chewing gum, or a toothpaste and applying the carrier to the dental tissue.
- the amorphous calcium phosphate compounds will recrystallize to the less soluble apatite form in the lesion and reform the tooth.
- the quantity of calcium and phosphate released is relatively low and, therefore, remineralization is slower than desirable.
- the aforementioned patents to Tung also teach the use of two-part solutions wherein a first part contains phosphate salt(s) and a second part contains calcium salts(s), wherein either the first part or the second part further contains carbonate salt(s).
- the Tung patents teach solutions formed by dissolving in water a solid powder containing calcium salt(s). These solutions are salt(s), and carbonate salt(s). These solutions are then applied to dental tissue.
- the Tung patents further teach the use of non-carbonated solid powders containing mixtures of calcium salts and phosphate salts which can be applied directly to the tooth or dispersed in gel, chewing gum, or other non-aqueous medium such as toothpaste which is placed in contact with the tooth.
- the patents teach that these powders are easily dissolved in saliva and then reprecipitated as an amorphous calcium phosphate compound.
- the Tung patents do not disclose the pHs of aqueous solutions formed from the non-carbonated solid powders.
- U.S. Pat. No. 5,605,677 discloses a toothpaste containing polishes, fluorine compounds, humectants, binders, and water, wherein the toothpaste is characterized in that it contains a combination of silica and dicalcium phosphate dihydrate at a weight ratio of 10:1 to 1:1 as the polishing component.
- the toothpaste taught therein restores the surfaces of teeth by providing controlled remineralization, particularly in scratch marks and dentinal canals. Such remineralization renders these areas substantially level, leaving the teeth with a smooth continuous surface. Schumann et al.
- the toothpaste therein may further contain magnesium ions and/or fluorophosphate ions.
- Schumann et al. does not disclose the presence of a water-soluble calcium compound in the toothpaste therein. Moreover, Schumann et al. does not teach the use of the magnesium ions to inhibit premature formation of calcium fluoride. The failure of Schumann et al. to teach this use of the magnesium ions therein is significant for reasons give hereinbelow.
- U.S. Pat. No. 5,603,922 discloses one-part and two-part products and methods of using same to remineralize subsurface lesions.
- the one-part and two-part products contain at least one water-soluble calcium salt, at least one water-soluble divalent metal salt wherein the divalent metal is other than calcium and at least one water-soluble phosphate salt.
- the divalent metal is preferably magnesium, strontium, tin or zinc.
- the calcium and divalent metal salts are disposed in a first discrete component, and the phosphate salt(s) is disposed in a second discrete component.
- the two-part product may further contain a dispensing means for allowing the first and second components to be simultaneously dispensed from the product so as to permit the dispensed first and second components to simultaneously contact the tooth or teeth being treated.
- the aqueous solution formed by mixing the salts used in the one-part and two-part products has a pH of from about 4.0 to about 7.0.
- U.S. Pat. No. 5,605,675 discloses a two-part product and method of using same for remineralizing dental enamel, wherein the product contains a first discrete component composed of at least one water-soluble calcium salt and a second discrete component composed of at least one water-soluble phosphate salt and at least one water-soluble fluoride salt.
- the first and second components are simultaneously dispensable from the product and each have a pH in water such that when the two components are mixed to form an aqueous mixed solution, the solution has a pH of from about 4.5 and 10.0.
- U.S. Pat. No. 5,571,502 (Winston et al.) is directed to one-part, non-aqueous products and methods of using same to remineralize subsurface lesions, wherein the products contain at least one water-soluble calcium slat; at least one water-soluble phosphate salt; either a stabilizer or a hydrophilic, non-aqueous, water-soluble vehicle; and, optionally, at least one water-soluble fluoride salt.
- the components When the components are mixed with water or saliva to form an aqueous mixed solution, the solution has a pH of from about 4.5 to about 10.0.
- Each of the products disclosed in the foregoing applications contains at least one water-soluble inorganic orthophosphate salt.
- Saliva itself helps protect teeth against demineralization and can slowly remineralize teeth which have become demineralized by acids. Because saliva is supersaturated with respect to calcium and phosphate ions, hydroxyapatite may be formed from substances occurring naturally in saliva. In the mouth, a natural equilibrium exists between the dissolution of hydroxyapatite from the teeth and the formation of hydroxyapatite on or in the teeth from the calcium and phosphate ions in the saliva. This equilibrium shifts continuously. If the equilibrium is such that hydroxyapatite is being dissolved, the result is demineralization and a carious condition. On the other hand, if the equilibrium is such that hydroxyapatite is being formed, remineralization occurs.
- fluoride ions can enhance the natural remineralization process, and this is one of the accepted mechanisms by which fluoride dentifrices protect against caries. Hydroxyapatite reacts with the fluoride ion and is thereby converted into fluoridated hydroxyapatite. Fluoridated hydroxyapatite is less soluble in an acid medium than is hydroxyapatite. Consequently, after a fluoride application, the tooth is better protected from the acid surges which initiate the caries process.
- the efficacy of fluoride-containing dentifrices to remineralize teeth is limited by the modes levels of free calcium and inorganic orthophosphate ions present in saliva.
- the concentration of free calcium ions in saliva is especially limited.
- the concentration of free calcium ions in parotid saliva varies from about 0.9 to about 1.5 millimoles per liter (36-60 parts per million (ppm)).
- the concentration of free inorganic orthophosphate ions in parotid saliva varies from about 3 to about 9 millimoles per liter (300-850 ppm) depending on the flow of the saliva. Since calcium hydroxyapatite and fluoroapatite contain a calcium-to-phosphate ion ratio of about 5:3, remineralization is most severely limited by the calcium ion levels in the saliva.
- compositions and methods designed to prevent the premature formation of calcium fluoride in dentifrice compositions are known in the art. Reference is made, for example, to U.S. Pat. Nos. 5,476,647 (Chow et al.); 4,283,385 (Dhabhar et al.); 4,923,683 (Sakuma et al.); 4,565,691 (Jackson); and 4,460,565 (Weststrate et al.).
- the Chow et al. patent teaches a two-part dentifrice product containing a soluble calcium source in one part and a soluble fluoride source in the other part, wherein reaction between the calcium and fluoride sources is avoided by incorporating a soluble calcium-complexing anion into the calcium part.
- the Dhabhar et al. patent teaches a dentifrice containing soluble fluoride and a calcium carbonate or calcium phosphate abrasive, wherein reaction between the fluoride and the abrasive is inhibited by the incorporation of an ethylenediaminetetraacetic acid or sodium salt thereof into the dentifrice.
- the Sakuma et al. patent discloses that the reaction between a hydroxyapatite compound and a fluoride compound in a dentifrice composition can be prevented by either storing the hydroxyapatite and fluoride compounds in separate receptacles or by coating or encapsulating one or both of the hydroxyapatite and fluoride compounds.
- reaction between a water-soluble ionic fluoride and an ionic calcium-containing abrasive in a dentifrice composition is reduced or prevented by including in the dentifrice composition a water-soluble ionic agent containing the anionic counter ions of the ionic abrasive and metal cations capable of forming a water-soluble fluoride.
- the Weststrate et al. patent teaches that a dentifrice composition containing two or more fluorine compounds, at least one soluble salt producing phosphate ions and at least one substance providing calcium ions, wherein inactivation of the fluoride and phosphate ions by the calcium ions is avoided by using specific calcium complexes as the source of calcium ions.
- Such calcium complexes include the calcium salts of organic acids, e.g., the calcium salts of citric acid, adipic acid, and tartaric acid.
- Calcium-enriched minerals such as calcium zeolite and calcium apofyllite are also suitable.
- a drawback to the processes taught in the aforementioned patents to Chow et al., Dhabhar et al. Sakuma et al. and Weststrate et al., is that the chelating, sequestering or otherwise supplying of calcium in bound form, e.g., hydroxyapatite, ties up the calcium and reduces its availability for remineralization when applied to the teeth.
- a drawback to the processes taught in the aforementioned patents to Jackson, and Schumann et al. is that providing the fluoride in complexed or bound form or even in the form of sodium monofluorophosphate reduces the availability of the fluoride for remineralization when applied to the teeth.
- the amount of inorganic orthophosphate ions in parotid saliva is substantially grater than the amount of calcium ions in the saliva. Since hydroxyapatite contains a 5:3 ration of calcium ions to inorganic orthophosphate ions and further because it is desirable to avoid premature formation of calcium phosphate in the dentifrice aqueous composition used to remineralize and/or mineralize the teeth, it would be desirable to provide a fluoride-containing dentifrice product which increases the concentration of free calcium ions in the remineralizing/mineralizing aqueous composition used to treat the teeth but which does not increase the level of free inorganic orthophosphate ions already present in the saliva. In other words, it would be desirable to provide a dentifrice product which contains fluoride and calcium compounds but which is substantially free of water-soluble inorganic orthophosphates.
- Dentifrice compositions containing calcium and fluoride compounds but free of water-soluble inorganic orthophosphate compounds are known in the art. Reference is made, for example, to U.S. Pat. Nos. 4,141,969 and 4,412,983 (both to Mitchell); 3,728,446 (Roberts et al.); 4,265,877 (Tenta); 4,983,379 (Schaeffer); 4,280,822 (Wason); 4,244,707 (Wason); 4,340,584 (Wason); and 5,045,305 (Clarkson et al.).
- U.S. Pat. Nos. 4,141,969 and 4,412,983 to Mitchell disclose dental cream compositions containing a dental vehicle, synthetic precipitated silica essentially free of alumina, a fluorine-providing compound and a water-soluble or water-insoluble calcium salt. Phosphate compounds may be present but are not required.
- the dental cream composition may further contain a metallic salt additive to provide metal ions in addition to the calcium ions.
- Magnesium salts, particularly water-soluble magnesium salts, such as magnesium chloride, are particularly desirable.
- U.S. Pat. No. 3,728,446 to Roberts et al. teaches a speckled dentifrice gel composition containing a gel vehicle composed of an aqueous liquid, an alkali metal carboxymethyl cellulose gelling agent, colored particles of the water-insoluble salt of carboxymethyl cellulose and a polyvalent metal, and, optionally, a soluble fluoride compound.
- the polyvalent metal which is provided as a water-soluble salt or water-soluble hydroxide, can be calcium, magnesium, strontium, barium, aluminum, gallium, germanium, tin, lead, iron, nickel, zinc, or cadmium.
- the composition may further contain a polishing agent such as, e.g., magnesium carbonate, calcium carbonate, dicalcium phosphate, tricalcium phosphate, insoluble sodium metaphosphate, calcium pyrophosphate, calcium sulfate and mixture thereof.
- a polishing agent such as, e.g., magnesium carbonate, calcium carbonate, dicalcium phosphate, tricalcium phosphate, insoluble sodium metaphosphate, calcium pyrophosphate, calcium sulfate and mixture thereof.
- U.S. Pat. No. 4,265,877 to Tenta is directed to a chewing gum composition containing a chewing gum base having distributed therein a mixture of sodium fluoride and calcium carbonate in the form of oyster shell.
- the oyster shell consists of about 97% of calcium carbonate and about 3% of a mixture of trace elements such as magnesium, silicon, manganese, iron, aluminum, copper, sodium, strontium, potassium and zinc.
- U.S. Pat. No. 4,983,379 to Schaeffer discloses a dental preparation containing a hydrogen peroxide-containing gel component and a sodium bicarbonate-containing paste component, the gel and paste components being separately stored but capable of being simultaneously dispensed from the package in which they are contained.
- the paste component may further contain a fluorine compound and cleansing agents such as calcium sulfate, calcium phosphate, calcium carbonate, magnesium carbonate, magnesium silicate, and mixtures of the foregoing.
- the paste component may also contain a polishing/stabilizing agent such as magnesium oxide.
- the alkaline earth metal may be calcium, magnesium or strontium, but is preferably calcium.
- the alkaline earth metal compound is water-soluble and includes the nitrates, oxides, hydroxides and chlorides.
- the polishing agent may be e.g., dicalcium phosphate, anhydrous dicalcium phosphate, tricalcium phosphate, thermally converted dicalcium phosphate, and insoluble sodium metaphosphate.
- U.S. Pat. No. 5,045,305 to Clarkson et al. teaches an oral hygiene product for inhibiting caries, which contains a first composition containing an aqueous solution of calcium ions and a second composition containing an aqueous solution of fluoride ions, wherein the first and second compositions are such that when mixed, rapid precipitation of calcium fluoride occurs.
- the oral hygiene product maintains a low fluoride ion concentration in the mouth for longer periods than conventional products by the rapid precipitation of calcium fluoride either in the mouth or immediately prior to use.
- a delivery system providing for physical separation of the two compositions and for simultaneous or sequential delivery of the compositions may also be used.
- dentifrice compositions containing calcium and fluoride compounds and free of water-soluble inorganic orthophosphate compounds, wherein such dentifrice compositions are capable of providing remineralization of subsurface lesions and/or mineralization of exposed dentinal tubules.
- a further object of this invention is to provide a fluoride-containing dentifrice product for remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules, wherein the dentifrice product further contains a source of calcium cations and is capable of adding calcium cations to the aqueous saliva composition used to treat the teeth.
- a still further object of this invention is to provide a dentifrice product for remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules, wherein the dentifrice product contains a source of fluoride ions and a source of calcium ions, wherein reaction between the fluoride and calcium sources to form calcium fluoride in the aqueous saliva composition used to treat the teeth is substantially delayed for a period of several minutes.
- Another object of this invention is to provide a dentifrice product for remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules, wherein the dentifrice product contains a source of fluoride ions and a source of calcium ions but is substantially free of soluble inorganic orthophosphates.
- Yet another object of this invention is to provide a product which has the foregoing characteristics and which is easily usable by the consumer and not differing significantly, in flavor and appearance, form customary dental cosmetics.
- a further object of this invention is to provide a method for remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules by means of a product having the aforementioned characteristics.
- the present invention is based on the discovery that, in an aqueous composition, the presence of a particular amount of at least one water-soluble or partially water-soluble magnesium compound can significantly delay the reaction between a water-soluble or partially water-soluble calcium compound and a water-soluble fluoride compound to form calcium fluoride if the magnesium and calcium compounds are combined with one another prior to being combined with the fluoride compound.
- fluoride ions can be introduced into the system without loss of free fluoride anions for up to several minutes.
- one embodiment of the present invention is directed to a two-art dentifrice product which is substantially free of soluble inorganic orthophosphates and which is capable of remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules in teeth, containing:
- the cationic and anionic parts each have a pH in eater such that a mixed aqueous composition formed by mixing the cationic and anionic parts with (i) saliva or (ii) water and saliva has a pH of from about 4.0 to about 10.0.
- Another embodiment of the present invention is directed to a two-part dentifrice product for remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules, containing:
- the cationic and anionic parts each have a pH in water such that a mixed aqueous composition formed by mixing the cationic and anionic parts with (i) saliva or (ii) water and saliva has a pH of greater than about 4.0 to about 10.0.
- a further embodiment of this invention is directed to a two-part dentifrice product for remineralizing subsurface lesions and/or mineralizing exposed dentinal tubules, containing:
- the product is substantially devoid of water-soluble inorganic orthophosphate compounds
- the cationic and anionic parts each have a pH in water such that a mixed aqueous composition formed by mixing the cationic and anionic parts with (i) saliva or (ii) water and saliva has a pH of from about 4.0 to about 10.0.
- the present invention is further directed to a method for remineralizing at least one subsurface lesion and/or mineralizing at least one exposed dentinal tubule in at least one tooth, involving the steps of:
- the products of this invention provide faster remineralization and/or mineralization. Furthermore, by adding such calcium cations while inhibiting the formation of insoluble calcium fluoride, the products of this invention provide faster remineralization and/or mineralization without sacrificing the degree of remineralization and/or mineralization achieved with fluoride.
- the present invention provides effective subsurface remineralization/mineralization at a faster rate without increasing the risk of premature formation of calcium phosphate in the remineralizing/mineralizing composition.
- the present invention provides dentifrice products capable of effecting remineralization of subsurface lesions and/or mineralization of exposed dentinal tubules, wherein the dentifrice products are easily usable by the consumer and do not differ significantly, in flavor and appearance, from customary dental cosmetics.
- the present invention provides dentifrice products and methods for remineralizing subsurface lesions in teeth and for mineralizing exposed dentinal tubules in teeth.
- disentifrice or “dentifrices” refers to products which remain in the mouth for a relatively short period of time, in which they are intimately contacted with substantially all surfaces of the teeth, and are then removed.
- Non-limiting examples of such products include toothpastes, prophylactic pastes, tooth polishes, gels, professional gels and other products applied by dentists, as well as mouth washes, rinses, dental flosses, chewing gums, lozenges, tablets, edible food products, and the like.
- the products of this invention are formulated as two discrete parts, i.e., a cationic part and an anionic part.
- the cationic part contains at least one water-soluble and/or partially water-soluble calcium compound and a fluoride-protecting amount of at least one water-soluble and/or partially water-soluble magnesium compound.
- the anionic part contains at least one water-soluble fluoride compound.
- the products of this invention are formulated as an anhydrous product in which the calcium and magnesium compounds are prevented from reacting during storage by the lack of available water.
- the ingredients may be further protected by coating or encapsulation techniques.
- the liquid carrier may be a non-aqueous solvent, preferably a non-aqueous solvent which is water-soluble or water-dispersible.
- the term "fluoride-protecting amount” means that amount of the magnesium compound which substantially delays reaction between the calcium and fluoride compounds in the mixed aqueous composition to form calcium fluoride, wherein the delay in such reaction is for a period of time sufficient to allow a sufficient number of the calcium cations and fluoride anions to diffuse through the tooth to the subsurface lesion and/or the exposed dentinal tubule to effect substantial subsurface remineralization and/or mineralization.
- such delay in reaction between the calcium and fluoride compounds to form calcium fluoride is at least about 10 seconds, and more preferably from about 10 seconds to about 3 minutes.
- the calcium and magnesium compounds are first mixed with one another before being mixed with the fluoride compound.
- the magnesium cations are able to "protect" the fluoride anions from the calcium cations for a period of time so as to substantially delay the formation of the sparingly soluble calcium fluoride.
- the delay in calcium fluoride formation allows the calcium cations added by the products of this invention to increase the rate of remineralization and/or mineralization rather than inactivate the soluble fluoride ions.
- the cationic and anionic parts are kept separate from one another until the product is to be used.
- the cationic and anionic parts coexist in the products of this invention in an unmixed state with respect to one another.
- the cationic and anionic parts can be prevented from reacting on storage by supplying them in an anhydrous mixture.
- the cationic part used in the product of this invention contains at least one water-soluble and/or partially water-soluble calcium compound and at least one water-soluble and/or partially water-soluble magnesium compound, while the anionic part contains at least one water-soluble fluoride compound.
- the term "partially water-soluble" with respect to the partially water-soluble calcium compound which can be used in the cationic part of the product of this invention refers to a calcium compound having a solubility which is greater than that of dicalcium phosphate dihydrate in an aqueous solution having a pH of about 7.0 and a temperature of about 25° C. but which is less than that solubility which would release more than about 1400 ppm of calcium cations in such aqueous solution.
- dicalcium phosphate dihydrate can release up to about 40 ppm of calcium cations by weight of the aqueous solution.
- calcium compounds useful in the cationic part of the product of this invention include calcium salts having a solubility in water such that the salt is capable of releasing more than about 40 ppm but no more than about 1400 ppm, preferably from about 100 ppm to no more than about 1400 ppm, of calcium cations by weight of an aqueous solution having a pH of about 7.0 at a temperature of about 25° C.
- partially water-soluble with respect to the partially water-soluble magnesium compound which can be used in the cationic part of the product of this invention refers to a magnesium compound having a solubility such that in an aqueous solution having a pH of about 7.0 and a temperature of about 25° C., the magnesium compound is capable of releasing more than about 40 ppm but no more than about 1400 ppm of magnesium cations, preferably from about 100 ppm to no more than about 1400 ppm of magnesium cations, by weight of the aqueous solution.
- water-soluble as used herein with respect to the water-soluble calcium, magnesium and fluoride compounds which can be used in the present invention refers to a solubility such that the compound is capable of releasing at least about 1400 ppm by weight of ions into an aqueous solution having a temperature of about 25° C. and a pH of about 7.0.
- Water-soluble calcium salts useful in the product of this invention include, for example, calcium chloride, calcium lactate, calcium nitrate, calcium acetate, and calcium gluconate.
- Non-limiting examples of calcium salts of partial water-solubility suitable for use in this invention include calcium sulfate, anhydrous calcium sulfate, calcium sulfate hemihydrate, calcium sulfate dihydrate, calcium malate, calcium tartrate, calcium malonate, calcium succinate, and mixtures of the foregoing. Calcium sulfate is preferred.
- the partially water-soluble calcium salt component of the products of this invention can be prepared in situ, for example, by preparing mixtures of an acid such as, e.g., tartaric acid, and a water-soluble calcium salt such as, e.g., calcium nitrate, and adjusting the pH as needed.
- an acid such as, e.g., tartaric acid
- a water-soluble calcium salt such as, e.g., calcium nitrate
- the principle known as the "common ion effect" can be used to control the solubility of the partially water-soluble calcium salt used in the present invention and to optimize calcium release and fluoride stability.
- a salt can be added to the product or solution of this invention wherein the anion of the salt is the same as the anion present in the calcium salt used in the particular product or solution.
- the sodium, potassium and ammonium salts are preferred for use to achieve the common ion effect.
- an anion which is part of another functional ingredient may also be added.
- the use of magnesium sulfate in a calcium sulfate-based formulation would supply at least some of the needed sulfate anion.
- Mixtures of water-soluble and partially water-soluble calcium salts may be used in the cationic part of the product of this invention.
- the product of this invention further contains a fluoride-protecting amount of at least one water-soluble and/or partially water-soluble magnesium compound in the cationic part of the product.
- the specific amount of the magnesium compound needed to protect the fluoride will generally depend on the solubility of the particular calcium compound used in the cationic part. In general, the more soluble the calcium compound, the greater the amount of magnesium compound is needed to protect the fluoride, while the less soluble the calcium compound, the lower the amount of magnesium compound is needed to protect the fluoride.
- the fluoride-protecting amount of the magnesium compound will preferably be that amount sufficient to provide an active magnesium ion concentration of at least about 0.05%, more preferably at least about 0.10% and most preferably from about 0.15% to about 0.5%, by weight based on the combined weight of the cationic and anionic parts. If the calcium compound is partially water-soluble, the fluoride-protecting amount of the magnesium compound will preferably be that amount sufficient to provide an active magnesium ion concentration of at least about 0.02%, more preferably at least about 0.05% and most preferably from about 0.07% to about 0.2%, by weight based on the combined weight of the cationic and anionic parts.
- Magnesium compounds suitable for use in the cationic part of the product of this invention include, for example, magnesium acetate, magnesium ammonium sulfate, magnesium benzoate, magnesium bromide, magnesium borate, magnesium citrate, magnesium chloride, magnesium chloride hexahydrate, magnesium gluconate, magnesium hydroxide, magnesium iodide, magnesium propionate, magnesium D-lactate, magnesium DL-lactate, magnesium phenolsulfonate, magnesium sulfate, magnesium nitrate, and magnesium tartrate.
- Preferred magnesium compounds are magnesium chloride and magnesium acetate. Magnesium oxide may also be used.
- magnesium oxide is very insoluble in water, it is preferably used in combination with an acid, an acid salt, or one or more buffers (e.g., a bicarbonate, which would reduce the pH of the magnesium oxide), so as to render the magnesium oxide partially water-soluble and therefore useful in the present invention.
- buffers e.g., a bicarbonate, which would reduce the pH of the magnesium oxide
- Suitable water-soluble fluoride compounds for use in the present invention include the alkali metal or ammonium fluorides such as sodium, potassium, lithium or ammonium fluoride; tin fluoride; indium fluoride; zirconium fluoride; copper fluoride; nickel fluoride; palladium fluoride; fluorozirconates such as sodium, potassium or ammonium fluorozirconate or tin fluorozirconate; fluorosilicates; fluoroborates; and fluorostannites.
- fluorophosphates such as sodium fluorophosphate, potassium fluorophosphate and ammonium fluorophosphate, are also suitable for use in the present invention.
- Sodium fluoride and stannous fluoride are the preferred fluoride compounds for use in the present invention.
- Organic fluorides such as the known amine fluorides, are also suitable for use in the products of the present invention.
- the cationic and anionic parts of the products of this invention each have a pH in water such that the mixed aqueous composition formed by mixing the two parts with saliva or with water and saliva has a pH ranging from about 4.0 to about 10.0, preferably from about 5.0 to about 9.0, more preferably from about 5.5 to about 8.5.
- the mixed aqueous composition used to treat the teeth in the present invention is composed of calcium cations released by the calcium compound(s), magnesium cations released by the magnesium compound(s), fluoride anions released by the fluoride compound(s), and inorganic orthophosphate anions provided by the saliva.
- the cationic and anionic parts are kept separate from one another until the product is to be used. Separation of the two parts can be achieved by various ways.
- the cationic and anionic parts may be separated by a physical barrier such as, for example, when the two parts are disposed in separate compartments of a two-compartment container, e.g., two-compartment tube or two-compartment aerosol can.
- a physical barrier such as, for example, when the two parts are disposed in separate compartments of a two-compartment container, e.g., two-compartment tube or two-compartment aerosol can.
- the two parts are kept separate from one another during storage but are preferably dispensed simultaneously with one another from the container.
- the cationic and anionic parts of the products of this invention may also be kept separate from each other by disposing the parts as separate layers in a multilayer product, for example, a two-layer mouthwash, a two-layer chewing gum, and the like.
- encapsulation materials include, e.g., shellac; waxes; fats; vinylpyridine; alkyl vinylpyridine and polymers/copolymers of other vinyl monomers; ethyl cellulose, benzyl cellulose, cellulose acetobutyrate and other cellulose derivatives; polyvinyl acetal diethylaminoacetate and dimethylaminoethyl methacrylate/methyl methacrylate copolymers; and the like.
- separation of the cationic and anionic parts may be achieved by disposing one part in an aqueous medium and the other part in a non-aqueous, water-insoluble medium, wherein the aqueous medium and the water-insoluble mediums are capable of simultaneously releasing the cationic and anionic parts.
- suitable non-aqueous mediums include non-aqueous solvents such as, e.g., ethyl alcohol, glycerine, propylene glycol and polyethylene oxide.
- the non-aqueous, hydrophilic liquid carrier medium is a polyethylene oxide having a molecular weight of about 400 (also known under the designation "Carbowax 400").
- Separation may also be achieved by disposing the two parts in a single carrier medium, wherein the single carrier medium is non-aqueous and hydrophilic and capable of simultaneously releasing the two parts upon contact with water.
- Yet another way to separate the cationic and anionic parts is to dispose the cationic part in a first carrier medium and the anionic part in a second carrier medium, wherein the first carrier medium is composed of a material in which the anionic part is insoluble but the cationic part is soluble, further wherein the second carrier medium is composed of a material in which the cationic part is insoluble but the anionic part is soluble.
- the cationic and anionic parts may both be aqueous, e.g., may both be in the form of aqueous solutions.
- one or both of the cationic and anionic parts may be non-aqueous.
- non-aqueous solvents may be employed in combination with water and/or saliva to form an aqueous/non-aqueous medium.
- Suitable non-aqueous solvents include, e.g., ethyl alcohol, glycerine, propylene glycol and polyethylene oxide.
- Solvent systems suitable for use in the present invention are those which are safe for use in the mouth.
- the anionic part of the product may contain a minor amount of a water-soluble inorganic orthophosphate salt.
- minor amount means that amount of the water-soluble inorganic orthophosphate compound such that a mixture of the water-soluble inorganic orthophosphate salt with the saliva with which it is combined to form the mixed aqueous composition has a concentration of inorganic orthophosphate ions of at least about 300 ppm but no higher than about 850 ppm. This concentration range is the average concentration range of inorganic orthophosphate anions in parotid saliva.
- Suitable water-soluble inorganic orthophosphate compounds for use in the present invention include, for example, the alkali salts and ammonium salts of orthophosphoric acid, such as, e.g., potassium, sodium or ammonium orthophosphate; monopotassium phosphate; dipotassium phosphate; tripotassium phosphate; monosodium phosphate; disodium phosphate and trisodium phosphate.
- orthophosphoric acid such as, e.g., potassium, sodium or ammonium orthophosphate
- monopotassium phosphate dipotassium phosphate
- tripotassium phosphate monosodium phosphate
- disodium phosphate disodium phosphate and trisodium phosphate.
- the product is substantially devoid of water-soluble inorganic orthophosphate compounds but may contain a water-insoluble phosphate compound as an abrasive and/or polishing agent.
- Suitable insoluble phosphate polishing agents include various calcium phosphates such as, for example, dicalcium phosphate, tricalcium phosphate, calcium pyrophosphate, beta-phase calcium pyrophosphate, dicalcium phosphate dihydrate, anhydrous calcium phosphate, sodium metaphosphate, and the like.
- a water-insoluble calcium phosphate polishing agent is used in the present invention, such polishing agent is preferably kept separate from the fluoride, particularly if the fluoride is sodium or stannous fluoride, so as to prevent formation of insoluble calcium fluoride during storage.
- the cationic and anionic parts are mixed either in the oral cavity or immediately prior to their introduction into the oral cavity. If the cationic and anionic parts are both aqueous compositions, the two parts may be mixed together outside of the oral cavity and the resulting mixture then immediately introduced into the oral cavity to be admixed with the saliva, the resulting saliva composition then being applied to the teeth. Alternatively, the two parts may be introduced into the oral cavity, where the two parts are combined simultaneously with one another and with the saliva to form the saliva composition used to treat the teeth.
- the two parts may be simultaneously introduced into the oral cavity, where they are chewed or sucked in the presence of saliva to form a saliva composition which is used to treat the teeth.
- the mixed aqueous composition formed by mixing the cationic and anionic parts with water and/or saliva has a pH of from about 4.0 to about 10.0, preferably from about 5.0 to about 9.0, more preferably from about 5.5 to about 8.5.
- a pH within such range enough of the calcium cations, magnesium cations, fluoride anions and inorganic orthophosphate anions remain soluble for the period of time required to remineralize the subsurface lesions and/or mineralize the exposed tubules of the dental enamel. If the mixed aqueous composition has a pH below about 3, demineralization will occur rapidly. A pH below about 2.5 is undesirable from a safety standpoint.
- the pH of the mixed aqueous composition may be adjusted to the desired pH by methods well known in the art.
- the pH may be lowered by the addition of any acid which is safe for use in the oral cavity and which yields the desired pH at the amount employed.
- suitable acids include acetic acid, phosphoric acid, citric acid and malic acid.
- the mixed aqueous composition and the insoluble precipitate formed therefrom in the present invention must both have acceptable levels of toxicity (i.e., the particular ions, in the amounts used in the remineralization/mineralization process, must be non-toxic) and must both be otherwise compatible in the oral environment.
- the cationic and anionic parts are delivered simultaneously to the tooth surfaces by means of the mixed aqueous composition.
- ions which effect remineralization and/or mineralization can be absorbed simultaneously by the dental enamel and their reaction causes re-hardening of the demineralized subsurface areas of the teeth and mineralization of the exposed dentinal tubules of the teeth.
- An important feature of the present invention lies in the mixing of the anionic and cationic parts and the "promptly applying" of the resulting mixed composition to the tooth.
- the term "promptly” as used herein with respect to the time period between mixing of the anionic and cationic parts in the presence of (i) saliva or (ii) water and saliva and the application of the mixed aqueous composition to the teeth means that time period which is sufficient to allow a sufficient amount of the cations and anions to diffuse through the surface of the tooth to the dentin and/or subsurface of the tooth so as to achieve substantial subsurface remineralization and/or mineralization.
- the time period between the mixing of the cationic and anionic parts and the application of the resulting mixed aqueous composition to the teeth should not exceed 1 minute, and preferably is less than 1 minute.
- the period of time of exposure of the mixed aqueous composition to the teeth must be great enough to allow the aforementioned diffusion of the ions into the demineralized subsurface to occur. Typically, at least about ten seconds are required for such diffusion.
- the mixed aqueous composition is applied to the teeth for from about 10 seconds to about 3 minutes.
- the pH of the mixed aqueous composition will rise due to natural factors after its introduction into the oral cavity. Precipitation of the cations and anions occurs during this rise in pH but after the ions have diffused into the demineralized tooth enamel.
- a therapeutic amount of the desired cations and anions is used in the mouth.
- the composition placed in the mouth should be such as to raise the calcium content in the saliva above the normal levels of about 50 ppm.
- the calcium content should be raised to above about 100 ppm, more preferably above about 200 ppm, and most preferably above about 400 ppm.
- the composition placed in the mouth should also be such as to raise the fluoride content in the saliva to above about 0.1 ppm, preferably above about 1 ppm, more preferably above about 10 ppm, and most preferably above about 100 ppm.
- the remineralizing-mineralizing precipitate formed in the present invention is a calcium phosphate or a hydroxyapatite (the natural constituent of tooth enamel) with incorporated fluoride and magnesium ions. Because of the presence of the fluoride ions in the mixed aqueous composition used in this invention, the remineralized enamel is more resistant to demineralization than was the original enamel. Therefore, use of the mixed aqueous composition in accordance with the present invention not only remineralizes the enamel but also renders such enamel more resistant to subsequent demineralization than was the original enamel.
- the products of this invention can be used in conventional forms, for example, in solution, paste or gel form or as a solid substance.
- the only requirement is that until use of the product, the part containing the calcium and magnesium compounds remains separate from the part containing the fluoride compound.
- the products of this invention are in the form of toothpastes, prophylactic pastes, tooth polishes, gels, professional gels, creams and other products applied by dentists, as well as mouthwashes, rinses, dental flosses, chewing gums, lozenges, tablets, edible food products, and the like.
- the products of this invention may contain conventional additives for dental and oral cosmetics.
- the products may contain flavoring agents, aroma agents, surfactants, astringents and preservatives.
- Suitable polishing agents include, e.g., calcium carbonate and various calcium phosphates such as, for example, dicalcium phosphate, tricalcium phosphate, calcium pyrophosphate, and the like.
- Suitable abrasives which can be used in the present invention include, for example, silica xerogels.
- Other conventional toothpaste abrasives can be used in the products of this invention, such as, e.g., beta-phase calcium pyrophosphate, dicalcium phosphate dihydrate, anhydrous calcium phosphate, calcium carbonate, zirconium silicate, and thermosetting polymerized resins.
- Silica aerogels and insoluble metaphosphates such as insoluble sodium metaphosphate can also be used. Mixtures of abrasives can be also be used. Silica xerogel abrasives are preferred.
- the total content of abrasive agent in the dentifrice is variable but will generally be up to about 90% by weight of the total composition. Generally, however, the abrasive will be present in an amount of from about 5% to about 60% by weight, preferably from about 20% to about 50% by weight, and most preferably from about 25% to about 45% by weight.
- the gel-forming agents usually used include known thickeners, e.g., the alkali salts of polyacrylic acid, and also preferentially dehydrated silicon dioxide gels of particle size of 2 to 20 microns and specific surface area of about 200 to 900 square meters per gram.
- any suitable surface active or detersive material may be included in the dentifrice products of this invention. Such materials are desirable to provide additional detersive, foaming and anti-bacterial properties depending upon the specific type of surface active material.
- These detergents are usually water-soluble organic compounds and may be anionic, nonionic or cationic in structure. It is usually preferred to use the water-soluble non-soap or synthetic organic detergents.
- Suitable detersive materials include, for example, the water-soluble salts of higher fatty acid monoglyceride monosulfate detergents (e.g., sodium coconut fatty acid monoglyceride monosulfate), higher alkyl sulfate (e.g., sodium lauryl sulfate), alkyl aryl sulfonate (e.g., sodium dodecyl benzene sulfonate), higher fatty acid esters of 1,2-dihydroxy propane sulfonate (e.g., sodium coconut fatty acid ester of 1,2-dihydroxy propane sulfonate), and the like.
- higher fatty acid monoglyceride monosulfate detergents e.g., sodium coconut fatty acid monoglyceride monosulfate
- alkyl sulfate e.g., sodium lauryl sulfate
- alkyl aryl sulfonate e.g., sodium dodec
- the various surface active materials may be used in any suitable amount, generally from about 0.05% to about 10% by weight, and preferably from about 0.5% to about 5% by weight of the dentifrice product.
- toothpaste, gel and cream products within the scope of this invention preferably further contain sudsing agents, binding agents, and/or humectants.
- An inorganic thickener such as hydrated silica may also be added.
- Suitable sudsing agents for use in the present invention include those which are reasonably stable and which form suds throughout the period of application.
- non-soap anionic or nonionic organic synthetic detergents are employed.
- examples of such agents include, e.g., water-soluble salts of alkyl sulfate having from 10 to 18 carbon atoms in the alkyl radical, such as sodium lauryl sulfate; water-soluble salts of sulfonated monoglycerides of fatty acids having from 10 to 18 carbon atoms, such as sodium monoglyceride sulfonate; salts of C 10 -C 18 fatty acid amides of taurine, such as sodium N-methyl taurate; salts of C 10 -C 18 fatty acid esters of isothionic acid; and substantially saturated aliphatic acyl amides of saturated monoaminocarboxylic acids having 2 to 6 carbon atoms, and in which the acyl radical contains 12 to 16 carbon atoms, such as sodium
- a binding material can be added to thicken and provide a desirable consistency to the products of the present invention.
- suitable thickening agents include, e.g., water-soluble salts of cellulose ethers, such as, for example, sodium carboxymethyl cellulose, hydroxypropyl cellulose, and hydroxyethyl cellulose.
- Natural gums such as gum karaya, gum arabic, carrageenan and gum tragacanth, can also be used.
- Colloidal magnesium aluminum silicate, silica aerogels, silica xerogels, fumed silica, or other finely divided silica can be used as part of the thickening agent for further improved texture.
- a preferred thickening agent is xanthan gum.
- humectant material in toothpaste or gel embodiments of the present invention to keep such products from hardening.
- Suitable humectants include, e.g., glycerine, sorbitol, polyethylene glycol, propylene glycol, and other edible polyhydric alcohols, as well as mixtures thereof.
- Toothpaste or gel products within the scope of this invention may also contain flavoring agents such as, for example, oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove.
- flavoring agents such as, for example, oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove.
- Toothpaste or gel products of the present invention may also contain sweetening agents such as, e.g., saccharin, dextrose, levulose, sodium cyclamate, and aspartame. Mixtures of sugar with a sweetener, e.g., sucralose, are also contemplated for use in the present invention.
- sweetening agents such as, e.g., saccharin, dextrose, levulose, sodium cyclamate, and aspartame.
- a sweetener e.g., sucralose
- the dentifrice products of the present invention in the form of a transparent or translucent gel. This is accomplished by matching the refractive index of the water-humectant system with the abrasives and inorganic thickeners if used.
- Mouthwashes and rinses generally contain an aqueous solution of ethyl alcohol and flavoring materials.
- the alcohol provides an antibacterial effect, solubilizes the flavoring materials and provides a pleasant mouth feeling.
- Alcohol-free mouthwashes are now, however, gaining in popularity.
- mouthwashes and rinses also contain additional antibacterial agents and humectants such as glycerine and sorbitol which give a moist feeling to the mouth.
- mouthwashes and rinses preferably contain from about 0 to about 30%, preferably from about 0 to about 20%, by weight of ethyl alcohol; from about 30% to about 90% by weight of water; from about 0 to about 20% by weight of glycerine or other humectant; from about 0 to about 0.1% by weight of an antibacterial agent; from about 0 to about 0.2% by weight of a soluble fluoride source; from about 0.01% to about 0.5% by weight of a sweetening agent; from about 0.01% to about 2.0% by weight of a flavoring agent; and from about 0.1% to about 1% by weight of an emulsifier-surfactant.
- Chewable tablets may be formulated in a manner similar to the aforementioned dentifrices. Since the tablets are packaged in a water-free state, the cationic and anionic parts can be safely included in the same tablet. The reaction between the cationic and anionic parts will begin after they are in contact with the saliva through the chewing action.
- a plurality of packaging methods may be employed in order to separately contain or store the cationic and anionic parts and provide effective dispensing thereof into the oral cavity.
- the cationic and anionic parts may be simultaneously dispensed from separate collapsible tubes preferably made of plastic, a plastic and metal laminate, etc.
- the tubes may be held together by banding or cementing, preferably along the corresponding ventral sides of the tubes.
- the two tubes may be constructed to have abutting, preferably flat, sidewall portions.
- the mouths of the tubes are usually sufficiently close so that sufficient quantities of the cationic and anionic parts of the toothpaste or gel may be simultaneously dispensed directly on the toothbrush with the tubes being capped separately.
- another packaging method involves loading the cationic and anionic parts of the paste or gel into separate compartments of the same collapsible composite tube, joined by a common orifice.
- Such composite tube has compartments separated by a divider which is firmly attached along substantially diametrically opposed portions of the sidewall, and corresponding portions of the head structure of the tube.
- the divider may be glued or welded to the sidewall and head structure of the tube during manufacture of the latter.
- the divider is preferably provided with a protruding portion which extends into the mouth of the tube until its edge is substantially flush with the rim of the mouth.
- a divider forms with the sidewall two separate compartments of substantially the same volume for storage of the cationic and anionic parts, respectively.
- the two tubes are "concentric".
- An inner tube lies within and parallel with an outer tube.
- the mouths of the tubes abut at the same point.
- Protrusions or the like are inserted between the inner and outer tubes so that the component contained in the outer tube can pass through an available space between the mouth of the outer tube and the mouth of the inner tube.
- the closures of this tube-within-a-tube (which can screw on the outer tube or simply be held by pressure) may, but does not have to be, equipped with an interior protrusion to fit in the inner tube in order to prevent premature intermixing of the two components at the mouth of the tube.
- the tubes of all the above embodiments are usually filled from the bottom and are subsequently sealed together by conventional techniques.
- Another alternative packaging arrangement is a pressurized container which is provided with two compartments and two spouts.
- the internal pressure of the compartments is maintained by a pressurized gas, i.e., nitrogen, at the bottom of each compartment.
- Operation of a mechanical actuator actuates valves which release the contents of the compartments through the spouts, causing discharge of the paste or gel components onto a brush.
- the mouthwash, rinse or similar liquid embodiments are maintained in a manner similar to the pastes or gels in that, during storage, each of the cationic and anionic parts are maintained separate from one another to prevent premature reaction.
- the liquid cationic and anionic parts can therefore be stored each in separate compartments of a dual-compartment dispenser.
- the dispenser usually includes a closure system containing, for example, an inclined crown portion, at least two pouring spouts extending upwardly from an upper surface of the crown portion, and a cover for securement to the crown portion.
- the cover is provided with closure means, for example, depending plugs, to close the closure.
- Each pouring spout is preferably provided with a vent opening in addition to product orifices in the spouts.
- the orifices can be positioned close together on the crown, all of which assists in achieving control over pouring.
- Transparent containers have proven to be the most satisfactory. Transparency aids a person's ability to accurately and controllably dispense relatively equal volumes from a dual-compartment dispenser. Transparent walled containers also serve a window function for gauging the amounts of liquid remaining in the dispenser. The walls of the containers can be scribed or otherwise calibrated to assist in dispensing the correct remineralizing amount of the mixed aqueous composition.
- Examples 1-7 and Controls A-C ten (10) two-part products were prepared having the formulations shown in Table I below.
- the cationic part (i.e., part A) of the product contained partially water-soluble calcium sulfate as the calcium salt.
- the anionic part of each product contained sodium fluoride as the fluoride salt and was free of water-soluble inorganic orthophosphates.
- the cationic part of the products prepared in Examples 1-7 further contained magnesium chloride hexahydrate, while the cationic part of the products of Controls A-C did not contain a magnesium compound or any other divalent metal compound.
- the cationic and anionic parts of the products were combined and mixed for one minute with deionized water in a ratio of one part product to three parts water.
- the solutions were filtered to remove undissolved fluoride.
- the concentration of free fluoride in the filtered solution was measured and the results set forth in Table I.
- Table I recites the concentration of the magnesium chloride hexahydrate.
- the active magnesium ion concentration of the recited amount of the magnesium chloride hexahydrate can be calculated by dividing the atomic weight of magnesium (i.e., 24) by the molecular weight of magnesium chloride hexahydrate (i.e., 203) and multiplying the resulting value by the recited concentration of the magnesium chloride hexahydrate.
- a concentration of 0.8% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.1% by weight; a concentration of 0.4% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.05% by weight; and a concentration of 0.2% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.025% by weight.
- Examples 1-7 show that, in Examples 1-7, the free fluoride levels in the mixed aqueous solution increased with increasing magnesium content.
- Controls A-C which used no magnesium in the cationic part of the products, the mixed aqueous solution had much lower free fluoride levels than similar mixtures containing magnesium chloride.
- Examples 1-7 and Controls A-C illustrate the advantage of using magnesium in the cationic part of the product to retain relatively high levels of free fluoride in the mixed aqueous solution formed when the cationic and anionic parts are mixed.
- Examples 8-15 and Controls D-F show the effect on free fluoride levels in the mixed aqueous solution when the cationic part contains water-soluble calcium lactate and magnesium chloride.
- eleven (11) two-part products were prepared having the formulations shown in Table II below.
- part B was free of orthophosphate inorganic orthophosphate compounds and contained sodium fluoride as the fluoride salt
- part A contained calcium lactate.
- the cationic part further contained magnesium chloride, while, in Controls D and E, the cationic part did not contain magnesium chloride or any other divalent metal salt.
- the cationic part of the Control F product contained strontium chloride.
- the cationic and anionic parts of the products were combined and mixed for one minute with deionized water in a ratio of one part product to three parts water.
- the solutions were filtered to remove undissolved fluoride.
- the concentration of free fluoride in the filtered solution was measured and the results set forth in Table II.
- the free fluoride levels remaining after the two parts of each product were mixed are set forth in Table II.
- Table II recites the concentration of the magnesium chloride hexahydrate.
- the active magnesium ion concentration of the recited amount of the magnesium chloride hexahydrate can be calculated as described hereinabove.
- a concentration of 0.25% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.03% by weight
- a concentration of 0.5% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.06% by weight
- a concentration of 1.0% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.12% by weight
- a concentration of 1.5% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.18% by weight
- a concentration of 2.0% by weight of magnesium chloride hexahydrate provides an active magnesium ion concentration of about 0.24% by weight.
- Examples 16 and 17 and Controls G-J compare the free-fluoride protecting ability of a magnesium salt with the free-fluoride protecting ability of various other divalent metal salts.
- examples 16 and 17 and Controls G-J six (6) two-part products were prepared, having the formulations set forth in Table III below.
- the calcium salt used was water-soluble calcium acetate, and the divalent metal salt used was magnesium chloride.
- the divalent metal salt was magnesium chloride.
- the divalent metal salt was strontium chloride.
- Control I zinc acetate was used as the divalent metal salt.
- Control J the divalent metal salt was stannous chloride.
- the cationic and anionic parts of the products were combined and mixed for one minute with deionized water in a ratio of one part product to three parts water.
- the solutions were filtered to remove undissolved fluoride.
- the concentration of free fluoride in the filtered solution was measured and the results set forth in Table III.
- the free fluoride levels remaining after the two parts of each product were mixed are also set forth in Table III.
- Table III recites the concentration of the magnesium chloride hexahydrate.
- the active magnesium ion concentration of the recited amount of the magnesium chloride hexahydrate can be calculated as described hereinabove.
- Examples 16 and 17 and Controls G-J show that although magnesium, strontium, zinc and tin are all divalent metals, magnesium has relatively high fluoride-protecting ability under the conditions existing in Examples 16 and 17, whereas strontium, zinc and tin have no fluoride-protecting ability under the same conditions.
- Examples 18-21 and Control K illustrate the effect on free fluoride levels when the cationic part of the product contains sodium monofluorophosphate (sodium MFP) while the anionic part contains sodium fluoride.
- sodium MFP sodium monofluorophosphate
- the anionic part contained sodium fluoride.
- the cationic part also contained magnesium chloride.
- the cationic part did not contain magnesium chloride or any other divalent metal salt.
- the cationic and anionic parts of the products were combined and mixed for one minute with deionized water in a ratio of one part product to three parts water.
- the solutions were filtered to remove undissolved fluoride.
- concentration of free fluoride in the filtered solution was measured and the results set forth in Table IV.
- the free fluoride levels and the free calcium levels present in the mixed aqueous solutions formed by combining the cationic and anionic parts in each example and control are set forth in Table IV.
- Table IV recites the concentration of the magnesium chloride hexahydrate.
- the active magnesium ion concentration of the recited amount of the magnesium chloride hexahydrate can be calculated as described hereinabove.
- monofluorophosphate is reasonable stable in the presence of calcium ions
- monofluorophosphate can be included in formulations containing free calcium ions as was done in the Part A formulations shown in Table IV.
- the test method used in the fluoride analyses is such as to only include fluoride as the free ion, not as monofluorophosphate.
- the sodium monofluorophospate added to each formulations adds an additional 570 ppm active fluoride to the system. The total active fluoride content was determined by adding 570 to the determined free fluoride content.
- Monofluorophosphate ion is considered to be active fluoride for the purposes of anti-cavity protection. However, while in this form, it is much less effective in promoting remineralization than fluoride ion itself.
- Table IV show that magnesium chloride additions results in increased levels of free fluoride. Table IV also shows that despite the maintenance of higher free fluoride levels, the addition of magnesium ion did not adversely reduce the free calcium concentration. In fact, higher free calcium concentrations were obtained in the presence of magnesium. This indicates that the magnesium will have a beneficial effect on remineralization and mineralization.
Abstract
Description
TABLE I ______________________________________ Examples 1-7 and Controls A-C: Formulations ______________________________________ Example No. Concentration (parts by weight) Ingredient 1 2 3 4 ______________________________________ Part A Glycerine 10 5 10 5 PEG 8 1 1 1 1 Methyl Paraben 0.025 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 0.025 CMC 0.5 0.9 0.5 0.9 Water 20.15 20.35 20.15 20.35 Sorbitol 5 10 5 10 Sodium Saccharin 0.3 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0.8 0.2 0.8 0.2 Titanium Dioxide 0.1 0.1 0.1 0.1 Calcium Sulfate 2.85 2.85 2.85 2.85 Hydrated Silica Abrasive 4.75 4.75 4.75 4.75 Hydrated Silica Thickener 3 3 3 3 Flavor 0.5 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.5 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 5.75 NaOH 0 0 0.2 0.2 Acetic Acid 0 0 0.3 0.3 Lactic Acid 0 0 0 0 CMC 0.45 0.45 0.45 0.45 Water 12 12 11.5 11.5 Sorbitol 21.65 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 0.15 NaF 0.25 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 0.75 TOTAL 100 100 100 100 pH 6.72 6.72 7.9 7.9 Free Fluoride (ppm) 1037 212 1113 354 ______________________________________ Example No. Concentration (parts by weight) Ingredient 5 6 7 ______________________________________ Part A Glycerine 10 10 5 PEG 8 1 1 1 Methyl Paraben 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 CMC 0.5 0.5 0.9 Water 20.15 20.55 20.35 Sorbitol 5 5 10 Sodium Saccharin 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0.8 0.4 0.2 Titanium Dioxide 0.1 0.1 0.1 Calcium Sulfate 2.85 2.85 2.85 Hydrated Silica Abrasive 4.75 4.75 4.75 Hydrated Silica Thickener 3 3 3 Flavor 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 NaOH 0.025 0.025 0.025 Acetic Acid 0 0 0 Lactic Acid 0.1 0.1 0.1 CMC 0.45 0.45 0.45 Water 11.875 11.875 11.875 Sorbitol 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 NaF 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 TOTAL 100 100 100 pH 6.41 6.41 6.41 Free Fluoride (ppm) 997 380 204 ______________________________________ Control Concentration (parts by weight) Ingredient A B C ______________________________________ Part A Glycerine 10 10 10 PEG 8 1 1 1 Methyl Paraben 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 CMC 0.5 0.5 0.5 Water 20.95 20.95 20.95 Sorbitol 5 5 5 Sodium Saccharin 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0 0 0 Titanium Dioxide 0.1 0.1 0.1 Calcium Sulfate 2.85 2.85 2.85 Hydrated Silica Abrasive 4.75 4.75 4.75 Hydrated Silica Thickener 3 3 3 Flavor 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 NaOH 0 0.2 0.025 Acetic Acid 0 0.3 0 Lactic Acid 0 0 0.1 CMC 0.45 0.45 0.45 Water 12 11.5 11.875 Sorbitol 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 NaF 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 TOTAL 100 100 100 pH 6.72 7.9 6.41 Free Fluoride (ppm) 113 118 159 ______________________________________
TABLE II ______________________________________ Examples 8-15 and Controls D-F: Formulations ______________________________________ Example No. Concentration (parts by weight) Ingredient 8 9 10 11 ______________________________________ Part A Glycerine 6.5 6.5 6.5 6.5 PEG 8 0 0 0 0 Methyl Paraben 0.025 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 0.025 CMC 0.5 0.5 0.5 0.5 Water 18.9 18.4 17.9 17.4 Sorbitol 10 10 10 10 Sodium Saccharin 0.3 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0.5 1 1.5 2 Strontium Chloride 0 0 0 0 Calcium lactate 1.75 1.75 1.75 1.75 Hydrated Silica Abrasive 7 7 7 7 Hydrated Silica Thickener 3 3 3 3 Flavor 0.5 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.5 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 5.75 NaOH 0.2 0.2 0.2 0.2 Acetic Acid 0.3 0.3 0.3 0.3 Lactic Acid 0 0 0 0 CMC 0.45 0.45 0.45 0.45 Water 11.5 11.5 11.5 11.5 Sorbitol 21.65 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 0.15 NaF 0.25 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 0.75 TOTAL 100 100 100 100 pH 7.68 7.68 7.68 7.68 Free Fluoride (ppm) 260 522 806 845 ______________________________________ Example No. Concentration (parts by weight) Ingredient 12 13 14 15 ______________________________________ Part A Glycerine 6.5 6.5 6.5 6.5 PEG 8 0 0 0 0 Methyl Paraben 0.025 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 0.025 CMC 0.5 0.5 0.5 0.5 Water 19.4 19.4 19.4 19.4 Sorbitol 10 10 10 10 Sodium Saccharin 0.3 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0.5 1 1.5 2 Strontium Chloride 0 0 0 0 Calcium lactate 1.75 1.75 1.75 1.75 Hydrated Silica Abrasive 7 7 7 7 Hydrated Silica Thickener 3 3 3 3 Flavor 0.5 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.5 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 5.75 NaOH 0.025 0.025 0.025 0.025 Acetic Acid 0 0 0 0 Lactic Acid 0.1 0.1 0.1 0.1 CNC 0.45 0.45 0.45 0.45 Water 11.875 11.875 11.875 11.875 Sorbitol 21.65 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 0.15 NaF 0.25 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 0.75 TOTAL 100.5 101 101.5 102 pH 6.23 6.23 6.23 6.23 Free Fluoride (ppm) 286 415 744 793 ______________________________________ Controls Concentration (parts by weight) Ingredient D E F ______________________________________ Part A Glycerine 6.5 6.5 6.5 PEG 8 0 0 0 Methyl paraben 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 CMC 0.5 0.5 0.5 Water 19.4 19.4 18.75 Sorbitol 10 10 10 Sodium Saccharin 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0 0 0 Strontium Chloride 0 0 0.65 Calcium lactate 1.75 1.75 1.75 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 3 3 3 Flavor 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 NaOH 0.2 0.025 0.2 Acetic Acid 0.3 0 0.3 Lactic Acid 0 0.1 0 CMC 0.45 0.45 0.45 Water 11.5 11.875 11.5 Sorbitol 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 NaF 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 TOTAL 100 100 100 pH 7.68 6.23 7.68 Free Fluoride (ppm) 143 140 158 ______________________________________
TABLE III ______________________________________ Examples 16 and 17 and Comparative Examples G-J: Formulations ______________________________________ Example No./Control Concentration (parts by weight) Ingredient 16 17 G ______________________________________ Part A Glycerine 8.25 8.25 8.25 Methyl Paraben 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 CMC 0.5 0.5 0.5 Water 18.4 17.9 19.4 Sorbitol 10 10 10 Sodium Saccharin 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 1 1.5 0 Strontium Chloride 0 0 0 Zinc Acetate 0 0 0 Stannous Chloride 0 0 0 Calcium Acetate 0.5 0.5 0.5 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 3 3 3 Flavor 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 NaOH 0.2 0.2 0.2 Acetic Acid 0.3 0.3 0.3 Lactic Acid 0 0 0 CMC 0.45 0.45 0.45 Water 11.5 11.5 11.5 Sorbitol 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 NaF 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 TOTAL 100 100 100 pH 7.47 7.45 7.6 Free Fluoride (ppm) 864 837 391 ______________________________________ Control Concentration (parts by weight) Ingredient H I J ______________________________________ Part A Glycerine 8.25 8.25 8.25 Methyl Paraben 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 CMC 0.5 0.5 0.5 Water 18.1 18.3 18.3 Sorbitol 10 10 10 Sodium Saccharin 0.3 0.3 0.3 MgCl.sub.2.H.sub.2 O 0 0 0 Strontium Chloride 1.3 0 0 Zinc Acetate 0 1.1 0 Stannous Chloride 0 0 1.1 Calcium Acetate 0.5 0.5 0.5 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 3 3 3 Flavor 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 NaOH 0.2 0.2 0.2 Acetic Acid 0.3 0.3 0.3 Lactic Acid 0 0 0 CMC 0.45 0.45 0.45 Water 11.5 11.5 11.5 Sorbitol 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 NaF 0.25 0.25 0.25 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 TOTAL 100 100 100 pH 7.5 6.38 4.76 Free Fluoride (ppm) 294 366 372 ______________________________________
TABLE IV ______________________________________ Examples 18-21 and Control K: Formulations ______________________________________ Example No. Concentration (parts by weight) Ingredient 18 19 20 ______________________________________ Part A Glycerine 6.5 6.5 6.5 Methyl Paraben 0.025 0.025 0.025 Propyl Paraben 0.025 0.025 0.025 CMC 0.5 0.5 0.5 Water 18.98 18.48 17.98 Sorbitol 10 10 10 Sodium Saccharin 0.3 0.3 0.3 MgCl.sub.2.6H.sub.2 O 0.5 1 1.5 Calcium Lactate 1.75 1.75 1.75 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 3 3 3 Sodium MFP 0.42 0.42 0.42 Flavor 0.5 0.5 0.5 Tween 20 0.5 0.5 0.5 Part B Glycerine 5.75 5.75 5.75 NaOH 0.2 0.2 0.2 Acetic Acid 0.3 0.3 0.3 CMC 0.45 0.45 0.45 Water 11.625 11.625 11.625 Sorbitol 21.65 21.65 21.65 Sodium Saccharin 0.15 0.15 0.15 NaF 0.125 0.125 0.125 Hydrated Silica Abrasive 7 7 7 Hydrated Silica Thickener 1.5 1.5 1.5 Flavor 0.5 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 0.75 TOTAL 100 100 100 pH 6.22 6.22 6.2 Free Fluoride (ppm) 181 291 528 Free Calcium (ppm) 1649 1944 1993 Total Active Fluoride (ppm) 751 861 1098 ______________________________________ Example No./Control Concentration (parts by weight) Ingredient 21 K ______________________________________ Part A Glycerine 6.5 6.5 Methyl Paraben 0.025 0.025 Propyl Paraben 0.025 0.025 CMC 0.5 0.5 Water 17.48 19.48 Sorbitol 10 10 Sodium Saccharin 0.3 0.3 MgCl.sub.2.6H.sub.2 O 2 0 Calcium Lactate 1.75 1.75 Hydrated Silica Abrasive 7 7 Hydrated Silica Thickener 3 3 Sodium MFP 0.42 0.42 Flavor 0.5 0.5 Tween 20 0.5 0.5 Part B Glycerine 5.75 5.75 NaOH 0.2 0.2 Acetic Acid 0.3 0.3 CMC 0.45 0.45 Water 11.625 11.625 Sorbitol 21.65 21.65 Sodium Saccharin 0.15 0.15 NaF 0.125 0.125 Hydrated Silica Abrasive 7 7 Hydrated Silica Thickener 1.5 1.5 Flavor 0.5 0.5 Sodium Lauryl Sulfate 0.75 0.75 TOTAL 100 100 pH 6.19 6.27 Free Fluoride (ppm) 635 166 Free Calcium (ppm) 2146 1410 Total Active Fluoride (ppm) 1205 736 ______________________________________
Claims (28)
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US08/832,827 US6159449A (en) | 1997-04-03 | 1997-04-03 | Dentifrice products and methods for remineralizing and/or mineralizing teeth |
PCT/US1998/000982 WO1998043602A1 (en) | 1997-04-03 | 1998-01-28 | Dentifrice products and methods for remineralizing and/or mineralizing teeth |
AU62434/98A AU6243498A (en) | 1997-04-03 | 1998-01-28 | Dentifrice products and methods for remineralizing and/or mineralizing teeth |
ARP980101517A AR011461A1 (en) | 1997-04-03 | 1998-04-03 | DENTAL PRODUCTS AND METHODS FOR REMINERALIZING AND / OR MINERALIZING TEETH |
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RU2816006C2 (en) * | 2018-07-05 | 2024-03-25 | Глаксосмиткляйн Консьюмер Хелскер (Юк) Айпи Лимитед | Dentifrice composition containing carboxylic acid or its alkali metal salt and source of free fluoride ions |
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ES2964951T3 (en) | 2018-01-22 | 2024-04-10 | Ivoclar Vivadent Ag | Procedure for remineralization of teeth |
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Also Published As
Publication number | Publication date |
---|---|
AU6243498A (en) | 1998-10-22 |
WO1998043602A1 (en) | 1998-10-08 |
AR011461A1 (en) | 2000-08-16 |
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